Small Organic Molecules Targeting PCAF Bromodomain as Potent Inhibitors of HIV-1 Replication

来源 :第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会 | 被引量 : 0次 | 上传用户：oliversong

【摘要】

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【作者】

：

Qiang Wang Ruirui Wang Baiqun Zhang Shuai Zhang Yongtang Zheng Zhiyong Wang

【机构】

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Hefei National Laboratory for Physical Sciences at Microscale,CAS Key Laboratory of Soft Matter Chem

【出处】

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第九届IUPAC化学生物学国际研讨会暨第八届世界华人药物化学研讨会

【发表日期】

：

2012年8期

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　　Human p300/CBP associated factor bromodomain(PCAF BRD),a relatively conserved host cell protein,can selectively bind with Tat-AcK50(tat acetylated lys50).This interaction is essential for the transcription activation of HIV-1 viral gene,therefore this PCAF BRD provides a potential targeting protein to inhibit the transcription.We synthesized a series of N1-ary1-propane-1,3-diamine compounds to bind to PCAF BRD.And cellular level anti-HIV-1 assay showed that these small molecules had good inhibitory potency on HIV-1 replication,which was consistent with the molecular assay.Also,it was found that 3-(2-nitrophenoxy) propan-1-amine derivatives had strong bioactivity against HIV-1 replication.

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Small Organic Molecules Targeting PCAF Bromodomain as Potent Inhibitors of HIV-1 Replication

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