Nagesh A Dhole

Publications (2)1.62 Total impact

• Article: Synthesis of new olefin chalcone derivatives as antitumor, antioxidant and antimicrobial agents

  Babasaheb P. Bandgar, Shivkumar S. Jalde, Laxman K. Adsul, Sadanand N. Shringare, Shrikant V. Lonikar, Rajesh N. Gacche, Nagesh A. Dhole, Shivraj H. Nile, Amol L. Shirfule
  [show abstract] [hide abstract]
  ABSTRACT: Chalcone is a unique template that is associated with several biological activities. Claisen–Schmidt condensation of olefin aldehyde 3 and various mono, disubstituted and heterocyclic acetophenones afforded novel olefin chalcones. Synthesized compounds were subjected for ADME prediction by computational method which revealed that these molecules can be considered as a potential drug. Out of the 21 compounds screened, compounds 5u, 5g, 5c and 5e have shown significant cytotoxicity against Hep 3BPN 7, compounds 5j, 5i, 5n and 5o showed good cytotoxicity against HL 60 P 58. Compounds 5f, 5c, 5e and 5b showed potent cytotoxicity against Hela B 75. Antioxidant activity was assessed using three methods, namely, 1,1-diphenyl-2-picrylhydrazyl (DPPH), hydroxyl radical scavenging and ferric reducing antioxidant power (FRAP). The result shows that all these compounds possess significant antioxidant activity. Compounds 5k, 5s, 5a and 5c showed promising antibacterial activity. Compounds 5k, 5u and 5f could be considered as chemopreventive agents.
  Medicinal Chemistry Research. 12/2012; 21(12):4512-4522.
• Article: Synthesis of novel carbazole chalcones as radical scavenger, antimicrobial and cancer chemopreventive agents.

  Babasaheb P Bandgar, Laxman K Adsul, Shrikant V Lonikar, Hemant V Chavan, Sadanand N Shringare, Sachin A Patil, Shivkumar S Jalde, Basawaraj A Koti, Nagesh A Dhole, Rajesh N Gacche, Amol Shirfule
  [show abstract] [hide abstract]
  ABSTRACT: A series of novel carbazole chalcones has been synthesised and evaluated for radical scavenging activity, cytotoxicity and antimicrobial activities. Compounds 12m, 12o and 12c exhibited good 2,2-diphenyl-1-picrylhydrazyl (DPPH) radical scavenging activity, compounds 12e, 12m and 12d were excellent hydroxyl radical scavengers and compounds 12a, 12e, 12g, 12n and 12m have shown inhibition of oxidative DNA damage induced by 2,2'-azobis (2-amidinopropane hydrochloride). Compounds 12j, 12i, 12n, 12c, 12m and 12e were most active against the selected cancer cell lines. Compounds 12a, 12e and 12m showed good antibacterial activity and compounds 12h and 12m have shown good antifungal activity. All the compounds were subjected for absorption, distribution, metabolism and excretion (ADME) predictions by computational method and found that these molecules could be considered as potential candidates for oral drug development.
  Journal of Enzyme Inhibition and Medicinal Chemistry 03/2012; · 1.62 Impact Factor