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Synthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells
Nie, LF (Nie, Li Fei);   Bozorov, K (Bozorov, Khurshed);   Niu, C (Niu, Chao);   Huang, GZ (Huang, Guozheng);   Aisa, HA (Aisa, Haji Akber); Aisa, HA
2017
Source PublicationRESEARCH ON CHEMICAL INTERMEDIATES
Volume43Issue:12Pages:6835-6843
Abstract

Phototherapy with psoralens as photosensitizers is the commonly used method for the treatment of vitiligo. Considering the structure similarity between psoralens and thieno[2,3-d]pyrimidinones, a series of novel sulfonamide derivatives containing tricyclic thieno[2,3-d]pyrimidinone were synthesized and evaluated for melanin synthesis in murine B16 cells. All new compounds were characterized by H-1 NMR, C-13 NMR, IR and HRMS (ESI). Among them, 6 compounds demonstrated excellent activity than positive control (8-methoxylpsoralen, 8-MOP) with more than 1.5-fold potency. Compound 11w with dichloro substitution at meta-positions in the benzenesulfonyl moiety was the most potent one (658.3 +/- 8.7%), exhibiting 5.0-fold stronger activity than 8-MOP (130.9 +/- 8.6%). The difluoro analog compound 11o increased melanin synthesis in murine B16 cells with a 4.35-fold potency as compared to 8-MOP. These compounds may serve as lead compounds for further drug discoveries for the treatment of vitiligo.

KeywordSulfonamide Thieno[2 Melanin Synthesis 3-d]Pyrimidinone Vitiligo
DOI10.1007/s11164-017-3023-3
Indexed BySCI
WOS IDWOS:000414497800005
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Document Type期刊论文
Identifierhttp://ir.xjipc.cas.cn/handle/365002/5018
Collection省部共建新疆特有药用资源利用重点实验室
Corresponding AuthorAisa, HA
AffiliationChinese Acad Sci, Xinjiang Tech Inst Phys & Chem, Key Lab Plant Resources & Chem Arid Reg, South Beijing Rd 40-1, Urumqi 830011, Peoples R China;Chinese Acad Sci, Xinjiang Tech Inst Phys & Chem, State Key Lab Basis Xinjiang Indigenous Med Plant, South Beijing Rd 40-1, Urumqi 830011, Peoples R China;Univ Chinese Acad Sci, Yuquan Rd 19 A, Beijing 100049, Peoples R China;Acad Sci Uzbek, Inst Chem Plant Subst, Mirzo Ulugbekstr 77, Tashkent 100170, Uzbekistan
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Nie, LF ,Aisa, HA. Synthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells[J]. RESEARCH ON CHEMICAL INTERMEDIATES,2017,43(12):6835-6843.
APA Nie, LF ,&Aisa, HA.(2017).Synthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells.RESEARCH ON CHEMICAL INTERMEDIATES,43(12),6835-6843.
MLA Nie, LF ,et al."Synthesis and biological evaluation of novel sulfonamide derivatives of tricyclic thieno[2,3-d]pyrimidin-4(3H)-ones on melanin synthesis in murine B16 cells".RESEARCH ON CHEMICAL INTERMEDIATES 43.12(2017):6835-6843.
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