Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents

	Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents
	Ashok P 1; Lu CL 2,3; Chander S 1; Zheng YT2; Murugesan S1; zhengyt@mail.kiz.ac.cn ; murugesan@pilani.bits-pilani.ac.in
	2015
发表期刊	CHEMICAL BIOLOGY & DRUG DESIGN
卷号	85 期号:6 页码:722-728
合作性质	其它
摘要	A novel series of 1-(thiophen-2-yl)-9H-pyrido [3,4-b]indole derivatives were synthesized using DL-tryptophan as starting material. All the compounds were characterized by spectral analysis such as H-1 NMR, Mass, IR, elemental analysis and evaluated for inhibitory potency against HIV-1 replication. Among the reported analogues, compound 7g exhibited significant anti-HIV activity with EC50 0.53m and selectivity index 483; compounds 7e, 7i, and 7o displayed moderate activity with EC50 3.8, 3.8, and 2.8m and selectivity index >105, >105, and 3.85, respectively. Interestingly, compound 7g inhibited p24 antigen expression in acute HIV-1(IIIB) infected cell line C8166 with EC50 1.1m. In this study, we also reported the Lipinski rule of 5 parameters, predicted toxicity profile, drug-likeness, and drug score of the synthesized analogues.
关键词	Aids C8166 Cells Haart Hiv-1 Indole P24 Antigen Beta-carboline
收录类别	SCI
文献类型	期刊论文
条目标识符	http://ir.kiz.ac.cn/handle/152453/8347
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	zhengyt@mail.kiz.ac.cn; murugesan@pilani.bits-pilani.ac.in
作者单位	1.Medicinal Chemistry Research Laboratory, Department of Pharmacy, Birla Institute of Technology and Science, Pilani, Rajasthan 333031, India 2.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, Yunnan 650223, China 3.Kunming College of Life Science, University of Chinese Academy of Sciences, Kunming, Yunnan 650204, China 4.Univ Chinese Acad Sci, Kunming Coll Life Sci, Kunming 650204, Yunnan, Peoples R China
推荐引用方式 GB/T 7714	Ashok P,Lu CL,Chander S,et al. Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents[J]. CHEMICAL BIOLOGY & DRUG DESIGN,2015,85(6):722-728.
APA	Ashok P.,Lu CL.,Chander S.,Zheng YT.,Murugesan S.,...&murugesan@pilani.bits-pilani.ac.in.(2015).Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents.CHEMICAL BIOLOGY & DRUG DESIGN,85(6),722-728.
MLA	Ashok P,et al."Design, Synthesis, and Biological Evaluation of 1-(thiophen-2-yl)-9H-pyrido[3,4-b]indole Derivatives as Anti-HIV-1 Agents".CHEMICAL BIOLOGY & DRUG DESIGN 85.6(2015):722-728.

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