Atta-ur- Rahman

Atta-ur- Rahman
University of Karachi · HEJ Research Institute of Chemistry

PhD (Cambridge), DSc (Cambridge), DSc (Coventry),

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1,136
Publications
107,403
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Publications

Publications (1,136)
Article
Seven known isoquinoline alkaloids 1-7 were isolated from the root extracts of Berberis parkeriana Schneid. Nine new derivatives 8-16 of one of the isolated compounds, jatrorrhizine (7), were synthesized. All the isolated as well as derivatized compounds were evaluated for their in-vitro acetylcholinesterase (AChE), and butyrylcholinesterase (BChE)...
Article
Full-text available
Phytochemical investigation of the trunk of Tabernaemontana contorta Stapf. led to the isolation and identifi�cation of two new glycocerebrosides, tabernamides A (1) and B (2), together with three known compounds: 2α,3α,23-trihydroxyursa-12,20(30)-dien-28-oic acid (3), 2α,3β, 23-trihydroxyursa-12,5(6)-dien-28-oic acid (4), and tombozine (5). All th...
Article
Three new constituents: 1,5R-dihydroxy-3,8S-dimethoxy-5,6,7,8-tetrahydroxanthone (1), (3S,4R,16S,17R)-3,16,23-trihydroxyoleana-11,13(18)-dien-28-aldehyde-3-O-β-D-glucopyranoside (2), and new natural product (S)-gentiandiol (3), along with 41 known compounds were isolated from Tujia ethnomedicine Shuihuanglian, namely, the whole plant of Swertia pun...
Patent
The present invention identifies new steroidal analogues of formestane synthesized through biotransformation with significant aromatase inhibitory activity, and thus can serve as possible safe, effective, and selective anti-cancer agent towards estrogen-responsive (ER+) breast cancer. Four new derivatives of anticancer drug formestane (1), 4α,5α,7α...
Patent
Four new analogues, 17β-hydroxy-7α,17α-dimethylestr-4,6-diene-3-one (2), 11β,17β-dihydroxy-7α, 17α-dimethyl-estra-1,3,5-triene-3-one (3), 3α,10β,17β-trihydroxy-7α,17α-dimethyl-5α-estrane (4), and 17β-hydroxy-7α,17α-dimethyl-5α-estrane-3,6-dione (5) of anabolic drug mibolerone (1) were synthesized. Derivatives 2 (IC50=3.83 ±0.3 μM) and 3 (IC50=4.24...
Article
Diabetes mellitus is a chronic metabolic disorder, with increasing prevalence and long-term complications. The aim of this study was to identify α-glucosidase inhibitory compounds with potential anti-hyperglycemic activity. For this purpose, a series of new clioquinol derivatives 2a-11a was synthesized, and characterized by various spectroscopic te...
Patent
New analogues of anti-cancer drugs atamestane (1), drostanolone enanthate ((3), and exemestane (6) were synthesized through biotransformation. New derivatives, 14α-hydroxy-1-methylandrosta-1,4-diene-3,17-dione ((2) (IC50, 9.7±0.72 nM) of 1 (IC50, 13.8±0.2 nM), and 2-methylandrosta-12β,17β-dihydroxy-1,4-diene-3-one (4) (IC50, 4.23±0.133 nM) of 3 (IC...
Article
Glomerella fusarioides-mediated structural modifications of steroidal anabolic drug, oxandrolone (1), yielded a new product 17β,11α-dihydroxy-17α-methylandrosta-2-oxa-4-ene-3-one (2). Similarly, Cunninghamella elegans-catalyzed transformation of a steroidal anti-epileptic drug ganaxolone (3) afforded a new metabolite 14α-hydroxy-5α-pregnan-1-ene-3,...
Article
Phytochemical investigation on the roots of Kadsura coccinea led to the isolation five previously unknown dibenzocyclooctadiene lignans, named heilaohusuins A-E (1-5). Their structures determined by NMR spectroscopy, HR-ESI-MS, and ECD spectra. Hepatoprotection effects of a series of dibenzocyclooctadiene derivatives (1-68) were investigated agains...
Patent
Biotransformation of an aromatase inhibitor, testolactone (1), yielded five new metabolites, 7α-hydroxy-3-oxo-13,17-secoandrosta-1,4-dieno-17,13α-lactone (2), 7β-hydroxy-3-oxo-13,17-seco-5β-androsta-1-eno-17,13α-lactone (3), 3α,11β-dihydroxy-13,17-seco-5β-androsta-17,13α-lactone (4), 4β,5β-epoxy-3β-hydroxy-13,17-secoandrosta-1-eno-17,13α-lactone (5...
Article
Full-text available
Anacyclus pyrethrum Lag. is a medicinal plant. In this study we evaluated the susceptibility of larvae of Aedes aegypti Linn. against potential larvicidal effects of root extract of A. pyrethrum. Bioassays were performed using World Health Organization methodologies. GC-MS analysis was employed to determine the contents of the extract. The underlyi...
Article
The identification of molecules, which could modulate protein-protein interactions (PPIs) is of primary interest to medicinal chemists. Using biophysical methods, we have screened 76 fragments (grouped into 16 mixtures) against the p8 subunit of the general transcription factor (TFIIH), which has recently been validated as an anti-cancer target. 10...
Article
Full-text available
A new pentacyclic triterpene 3-O-β-(E)-(4-O-acetylferuloyl)-lupeol (1) possessing an unusual (E)-acetylferuloyl moiety at C-3 and a new bicoumarin 7,7′-dimethoxy-6,6′-dicoumarinyl ether (2) were isolated from the liana Landolphia lucida K. Schum, along with fourteen previously known compounds 3-16, where methandriol dipropionate (3) and 2,3-bis-(4-...
Article
Ethnopharmacological relevance Schefflera is the largest genus in the family Araliaceae, which contains 602 known species indigenous to Asia, Africa, and the southwest Pacific region, several of which are used in traditional medicine. Aim of the review: The review discusses current knowledge of the traditional uses, phytochemistry, and biological a...
Article
Glomerella fusaroide, and Rhizopus stolonifer were effectively able to transform the steroidal hormone melengestrol acetate (MGA) (1) into four (4) new metabolites, 17α-acetoxy-11α-hydroxy-6-methyl-16-methylenepregna-4,6-diene-3,20-dione (2), 17α-acetoxy-11α-hydroxy-6-methyl-16-methylenepregna-1,4,6-triene-3,20-dione (3), 17α-acetoxy-6,7α-epoxy-6β-...
Article
Bletilla striata belongs to the family Orchidaceae, and it is mainly distributed in East Asia. The tubers of B. striata have been utilized in Traditional Chinese Medicine for various ailments, such as hematemesis, tuberculosis, malignant ulcers, hemorrhoids, traumatic bleeding, and chapped skin. Phytochemical investigation on B. striata has resulte...
Article
Full-text available
The incidence of 2019 novel corona virus (SARS-CoV-2) has created a medical emergency throughout the world. Various efforts have been made to develop the vaccine or effective treatments against the disease. The discovery of crystal structure of SARS-CoV-2 main protease has made the in silico identification of its inhibitors possible. Based on its c...
Article
A new steroidal alkaloid, michainine (1), was isolated from Fritillaria michailovskyi Fomin, along with nine known compounds 2–10 of different classes, including ribonucleoside, steroids, and fatty acids, which were isolated for the first time from this plant. Their structures were elucidated through extensive spectroscopic techniques, as well as b...
Article
Full-text available
Natural products have served as primary remedies since ancient times due to their cultural acceptance and outstanding biodiversity. To investigate whether Tamarix aphylla L. modulates an inflammatory process, we carried out bioassay-guided isolation where the extracts and isolated compounds were tested for their modulatory effects on several inflam...
Article
Kadsura heteroclita Roxb. Craib. (Schisandraceae), is a vine plant mainly distributed in southwest part of China. A new dibenzocyclooctadiene lignan, kadsulignan W (1), along with eleven known lignans (2–12) were isolated from chloroform soluble fraction of stems of Kadsura heteroclita. The structure of new lignan was elucidated by extensive spectr...
Article
Candida albicans is the causative agent of candidiasis in immunocompromised and diseased individuals. The current study was designed to evaluate the antifungal activity of Trachyspermum ammi (L.) Sprague seeds ethanolic extract and hexanes fraction against Candida albicans, both in-vitro and in-vivo. The minimal inhibitory concentration of hexanes...
Article
Seven new derivatives, 6α-hydroxy-1-methyl-3-oxo-5α-androst-1-en-17-yl acetate (2), 6α,17β-dihydroxy-1-methyl-3-oxo-5α-androst-1-en (3), 7β-hydroxy-1-methyl-3-oxo-5α-androst-1-en-17-yl acetate (4), 15β,20-dihydroxy-1-methyl-3-oxo-5α-androst-1-en-17-yl acetate (5), 15β-hydroxy-1-methyl-3-oxo-5α-androst-1-en-17-yl acetate (6), 12β,17β-dihydroxy-1-met...
Article
Full-text available
Xuetonglactones A-F (1-6), six unreported highly oxidized lanostane-and cycloartane-type triterpenoids along with 22 known scaffolds (7-28) were isolated from the stems of Kadsura heteroclita (Roxb.) Craib. Compared with previous congeners, xuetonglactone A (1), possesses an unprecedented 20,21-α-epoxide, and xuetonglactone D (4) features an unusua...
Article
Full-text available
The present study reports the biotransformation of an anabolic-androgenic steroid (AAS) drostanolone heptanoate (1) by using two microbial cultures, Beauveria bassiana, and Macrophomina phaseolina. Fermentation of 1 with B. bassiana yielded five new transformed products 2–6, while with M. phaseolina it afforded two new 7–8, and two known 9–10 metab...
Article
Full-text available
Cucurbitaceae is an important plant family because many of its species are consumed as food, and used in herbal medicines, cosmetics, etc. It comprises annual vines and is rich in various bioactive principles which include the cucurbitacins. These steroidal natural products, derived from the triterpene cucurbitane, are mainly the bitter principles...
Article
In the present work, we reported the triterpenoids isolated from n-butanol fraction of Kadsura heteroclita which is a Tujia ethnomedicine with trivial name "Xuetong". This effort resulted in the isolation of six unpresented triterpenoids xuetongsu A-F (1-6), along with five known triterpenoids (7-11). The structures of the reported compounds were e...
Article
Full-text available
Plants have so much to offer as far as the discovery of new bioactive molecules is concerned. Among the several classes of phytochemicals, xanthones offer greater structural diversity and pharmacological value. They are variable but definitely antioxidant in nature. Thus they are attractive targets for natural product and medicinal chemists. Xantho...
Article
Full-text available
As part of our continual efforts to exploit ‘Tujia Ethnomedicine’ for their pharmacophoric functionalities, we herein investigated Kadsura heteroclita collected from a deep Wulin mountain area in northern Hunan province. The current study resulted in the isolation of three new sesquiterpenes: 6α,9α,15-trihydroxycadinan-4-en-3-one (1), (+)-3,11,12-t...
Article
Full-text available
Biotransformation of a synthetic progestonic hormone dydrogesterone (1), C21H28O2, with a plant pathogenic fungus Macrophomina phaseolina yielded two new 2 and 3, and a known 4 metabolites. These analogues were identified as, 3β,11α-dihydroxy-5β,9β,10α-pregna-7-ene-6,20-dione (2), 15β-hydroxy-9β,10α-pregna-4,6-diene-3,20-dione (3), and 8α-hydroxy-9...
Article
Full-text available
Sulfamethazine (SMZ) (1) is an antibacterial sulfa drug which suppresses the synthesis of dihydrofolic acid. It is used for the treatment of infections in livestock; such as gastrointestinal, and respiratory tract infections. During the current study, synthesis, characterization, and evaluation of immunomodulatory activities of derivatives of sulfa...
Data
Spectral data of compound 5. (PDF)
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Spectral data of compound 9. (PDF)
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Spectral data of compound 11. (PDF)
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Spectral data of compound 16. (PDF)
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Spectral data of compound 20. (PDF)
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Spectral data of compound 24. (PDF)
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Spectral data of compound 29. (PDF)
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Spectral data of compound 33. (PDF)
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General reaction for the synthesis of compounds 3–39. (TIF)
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Spectral data of compound 4. (PDF)
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Spectral data of compound 7. (PDF)
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Spectral data of compound 10. (PDF)
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Spectral data of compound 13. (PDF)
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Spectral data of compound 15. (PDF)
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Spectral data of compound 18. (PDF)
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Spectral data of compound 19. (PDF)
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Spectral data of compound 21. (PDF)
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Spectral data of compound 22. (PDF)
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Spectral data of compound 23. (PDF)
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Spectral data of compound 27. (PDF)
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Spectral data of compound 31. (PDF)
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Spectral data of compound 37. (PDF)
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Spectral data of compound 38. (PDF)
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Spectral data of compound 39. (PDF)
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Institutional ethical committee approval. (PDF)
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Spectral data of compound 3. (PDF)
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Spectral data of compound 8. (PDF)
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Spectral data of compound 17. (PDF)
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Spectral data of compound 25. (PDF)
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Spectral data of compound 30. (PDF)
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Spectral data of compound 35. (PDF)
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Spectral data of compound 36. (PDF)
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Spectral data of compound 6. (PDF)
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Spectral data of compound 12. (PDF)
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Spectral data of compound 14. (PDF)