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ABSTRACT: A variety of diazepinone derivatives were prepared from α-amino acids and amino alcohols by a new synthetic methodology based on ring closing metathesis as a key step. The diazepinones were coupled with ribose derivatives to afford novel diazepinone nucleosides. Among them, (4R)-1-ribosyl-4-methyl-3,4-dihydro-1H-1,3-diazepin-2(7H)-one () showed a potent inhibitory effect (K(i) = 145.97 ± 4.87 nM) against human cytidine deaminase.
Chemical Communications 10/2012; · 6.17 Impact Factor
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ABSTRACT: The natural products moracins O and P exhibited potent in vitro inhibitory activity against hypoxia-inducible factor (HIF-1), which is a key mediator during adaptation of cancer cells to tumour hypoxia. Systematic variations of the structures of benzofuran type moracins were made and structure-activity relationship analysis showed the importance of the 2-arylbenzofuran ring and the (R)-configuration of the core scaffold. Further evaluation of the representative compound 5 showed its inhibitory effect on HIF-1α protein accumulation and target gene expression under hypoxia.
European journal of medicinal chemistry 06/2011; 46(6):2386-96. · 3.27 Impact Factor
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Kyung Hoon Min,
Yan Xia,
Eun Kyung Kim,
Yinglan Jin, Navneet Kaur,
Eun Seon Kim,
Dae Kyong Kim,
Hwa Young Jung,
Yongseok Choi,
Mi-Kyung Park,
Yong Ki Min,
Kiho Lee,
Kyeong Lee
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ABSTRACT: Novel disubstituted adamantyl derivatives were synthesized and evaluated in a P-glycoprotein dependent multidrug resistance cancer cell line. The hit to lead optimization provided potent MDR reversal agents. Some potent adamantyl derivatives were more than 10-fold more potent than verapamil without considerable intrinsic cytotoxicity. The 3-trifluorophenyl derivative 14f did not affect the metabolism of CYP450 3A4, whereas most of MDR revertants had a weak inhibitory effect.
Bioorganic & medicinal chemistry letters 09/2009; 19(18):5376-9. · 2.65 Impact Factor
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ABSTRACT: The first total synthesis of the naturally occurring benzofurans, moracins O and P was achieved using a Sonogashira cross coupling reaction followed by in situ cyclization, and the absolute configuration of natural moracin O was established.
Chemical Communications 05/2009; · 6.17 Impact Factor
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Eun Young Song, Navneet Kaur,
Mi-Young Park,
Yinglan Jin,
Kyeong Lee,
Guncheol Kim,
Ki Youn Lee,
Jee Sun Yang,
Jae Hong Shin,
Ky-Youb Nam,
Kyoung Tai No,
Gyoonhee Han
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ABSTRACT: A series of amide and urea derivatives of benzothiazole have been synthesized and evaluated for their antiproliferative profile in human SK-Hep-1 (liver), MDA-MB-231 (breast), and NUGC-3 (gastric) cell lines. Among them, compounds 1-2, 16-18, 23, and 25-26 had potent to moderate inhibitory activities. Further these compounds were investigated for their ability to inhibit Raf-1 activity.
European Journal of Medicinal Chemistry 08/2008; 43(7):1519-24. · 3.35 Impact Factor
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Kyeong Lee,
Jung S Ryu,
Yinglan Jin,
Woncheol Kim, Navneet Kaur,
Sang J Chung,
Yong-Jin Jeon,
Joon-Tae Park,
Ji S Bang,
Hong S Lee,
Tae Y Kim,
Jung J Lee,
Young-Soo Hong
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ABSTRACT: A new series of geldanamycin derivatives were synthesized using a semi-synthetic approach involving genetically engineered biosynthetic intermediates. These analogues were then evaluated for anti-proliferation activity in human cancer cell lines, SK-Br3 and SK-Ov3. Most of the synthesized compounds exhibited potent in vitro anti-proliferation activity toward both cell lines. Such compounds potently inhibited the expression of the Hsp90 client protein ErbB2.
Organic & Biomolecular Chemistry 02/2008; 6(2):340-8. · 3.70 Impact Factor
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Eun Young Song, Navneet Kaur,
Mi-Young Park,
Yinglan Jin,
Kyeong Lee,
Guncheol Kim,
Ki Youn Lee,
Sun Jee,
Yang,
Jae Hong Shin,
Ky-Youb Nam,
Kyoung Tai No,
Gyoonhee Han
[show abstract]
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ABSTRACT: A series of amide and urea derivatives of benzothiazole have been synthesized and evaluated for their antiproliferative profile in human SK-Hep-1 (liver), MDA-MB-231 (breast), and NUGC-3 (gastric) cell lines. Among them, compounds 1e2, 16e18, 23, and 25e26 had potent to moderate inhibitory activities. Further these compounds were investigated for their ability to inhibit Raf-1 activity.
