Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors

	Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors
	Ma XD 1; Zhang X 4,5; Yang SQ 1; Dai HF 3; Yang LM 4; Gu SX 1; Zheng YT 4; He QQ 1; Chen FE*1,2; rfchen@fudan.edu.cn
	2011
发表期刊	Bioorganic & Medicinal Chemistry
卷号	19 期号:16 页码:4704-4709
摘要	A series of (+/-)-benzhydrol derivatives featuring the essential sulfonamide group at the para position on the C-ring were synthesized and evaluated for the potential anti-HIV activity in C8166 cells. Most of these analogues demonstrated low concentration inhibitory activity with EC(50) values less than 1 mu M against the wild-type HIV-1. In particular, compound 7h was identified as the highest active inhibitor of wildtype HIV-1 with an EC(50) value of 0.12 mu M and selectivity index value of 312.73. Furthermore, some of them also exhibited moderate activity against the double mutant strain A(17) (K103N + Y181C) with EC(50) values lower than 5 mu M. In addition, the binding modes with RT and the preliminary structure-activity relationships of these derivatives were also explored for further chemical modifications.
关键词	Hiv Nnrtis Benzophenone Derivatives Benzhydrol Sar
资助者	This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029). ; This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029). ; This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029). ; This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029).
收录类别	SCI
语种	英语
资助者	This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029). ; This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029). ; This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029). ; This work was supported in part by grants from the National Natural Science Foundation of China (Nos. 20872018 and 30672536), the National Natural Science Foundation of Shanghai (No. 10ZR1401900), the Knowledge Innovation Program of CAS (KSCX2-YW-R-185), 973 program (2009CB522306) and Eleventh Five-Year Key Scientific and Technological Program of China (2009ZX09501-029).
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/353002/6660
专题	科研部门_分子免疫药理学（郑永唐）科研部门_动物模型与人类重大疾病机理重点实验室
通讯作者	rfchen@fudan.edu.cn
作者单位	1.Department of Chemistry, Fudan University, Shanghai 200433, PR China 2.Institute of Biomedical Science, Fudan University, Shanghai 200433, PR China 3.School of Pharmacy, Fudan University, Shanghai 200031, PR China 4.Key Laboratory of Animal Models and Human Disease Mechanisms of Chinese Academy of Sciences & Yunnan Province, Kunming Institute of Zoology, Chinese Academy of Sciences, Kunming 650223, PR China 5.Graduate School of the Chinese Academy of Sciences, Beijing 100039, PR China
推荐引用方式 GB/T 7714	Ma XD,Zhang X,Yang SQ,et al. Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors[J]. Bioorganic & Medicinal Chemistry,2011,19(16):4704-4709.
APA	Ma XD.,Zhang X.,Yang SQ.,Dai HF.,Yang LM.,...&rfchen@fudan.edu.cn.(2011).Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors.Bioorganic & Medicinal Chemistry,19(16),4704-4709.
MLA	Ma XD,et al."Synthesis and biological evaluation of (+/-)-benzhydrol derivatives as potent non-nucleoside HIV-1 reverse transcriptase inhibitors".Bioorganic & Medicinal Chemistry 19.16(2011):4704-4709.

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