Synthesis and structure–activity relationship of botryllamides that block the ABCG2 multidrug transporter
摘要:
In previous work, botryllamides discovered from the marine ascidian Botryllus tyreus were characterized as selective inhibitors of the ABCG2 multidrug transporter. However, the structural basis for this activity could not be established. In this study, botryllamide F, the core botryllamide structure, and botryllamide G, the most potent botryllamide ABCG2 inhibitor, were synthesized along with a series of structural variants for evaluation of structure - activity relationships. The biological activity of synthetic botryllamide analogs implied that the 2-methoxy-p-coumaric acid portion, and the degree of double bond conjugation within this group, were critical for inhibition of ABCG2. However, variations in the substituents on the two aryl groups did not appear to significantly impact the potency or degree of inhibition. (C) 2010 Elsevier Ltd. All rights reserved.
The imino‐Nazarov cyclization of the polysubstituted pentan‐1,4‐diene‐3‐imines was realized. To this aim, a one‐pot procedure involving reductive alkenyliminylation of α,β‐unsaturated secondary amides with potassium organotrifluoroborates, followed by acid‐catalyzed imino‐Nazarov cyclization of the polysubstituted pentan‐1,4‐diene‐3‐imine intermediates, was studied systematically. This mild, operationally
The present invention relates to symmetric diesters of hydroxyalkyl-4-hydroxy- tetraalkylpiperidine compounds and their use as light stabilizers. They are compatible with and soluble in coating formulations of different polarity.
Ultraviolet absorbing lenses and methods of making the same
申请人:CIBA-GEIGY AG
公开号:EP0388356A2
公开(公告)日:1990-09-19
An ultraviolet radiation absorbing contact or intraocular lens and method of making the same, comprising a polymeric lens material to which is covalently bonded at least one halotriazine reactive ultraviolet radiation absorbing agent of the formula
wherein A and E₂ are ultraviolet radiation absorbing groups which are either identical to or dissimilar to each other, or of the formula IB
wherein X is Cl or F; A is an ultraviolet radiation absorbing group; and E₁ is an aqueous soluble group.
一种紫外线辐射吸收隐形眼镜或眼内透镜及其制造方法,包括一种聚合透镜材料,其上共价键合有至少一种卤三嗪反应型紫外线辐射吸收剂,其式为
其中 A 和 E₂ 是彼此相同或不同的紫外线辐射吸收基团,或式 IB
其中 X 是 Cl 或 F;A 是紫外线辐射吸收基团;E₁ 是水溶性基团。
POLYBORATE COINITIATORS FOR PHOTOPOLYMERIZATION
申请人:Ciba Specialty Chemicals Holding Inc.
公开号:EP0983277A1
公开(公告)日:2000-03-08
PROCESS FOR THE PRODUCTION OF PHOSPHOR ORGANIC COMPOUNDS