Structure–anticancer activity relationships among 4-azolidinone-3-carboxylic acids derivatives

• Дата: 2010
• Автори: Kaminskyy, D.V., Lesyk, R.B.
• Формат: Стаття
• Мова: English
• Опубліковано: Інститут молекулярної біології і генетики НАН України 2010
• Назва видання: Вiopolymers and Cell
• Теми: Bioorganic Chemistry
• Онлайн доступ: http://dspace.nbuv.gov.ua/handle/123456789/153871
• Назва журналу: Digital Library of Periodicals of National Academy of Sciences of Ukraine
• Цитувати: Structure–anticancer activity relationships among 4-azolidinone-3-carboxylic acids derivatives / D.V. Kaminskyy, R.B. Lesyk // Вiopolymers and Cell. — 2010. — Т. 26, № 2. — С. 136-145. — Бібліогр.: 35 назв. — англ.

The aim of present research was investigation of anticancer activity of 4-azolidinone-3-carboxylic acids derivatives, and studies of structure–activity relationships (SAR) aspects. Methods. Organic synthesis; spectral methods; anticancer screening was performed according to the US NCI protocol (Developmental Therapeutic Program). Results. The data of new 4-thiazolidinone-3-alkanecarboxylic acids derivatives in vitro anticancer activity were described. The most active compounds which belong to 5-arylidene-2,4- thia(imida)zolidinone-3-alkanecarboxylic acids; 5-aryl(heteryl)idenerhodanine-3-succinic acids derivatives were selected. Determination of some SAR aspects which allowed to determine directions in lead-compounds structure optimization, as well as desirable molecular fragments for design of potential anticancer agents based on 4-azolidinone scaffold were performed. 5-Arylidenehydantoin-3-acetic acids amides were identified as a new class of significant selective antileukemic agents. Possible pharmacophore scaffold of 5-ylidenerhodanine-3-succinic acids derivatives was suggested. Conclusions. The series of active compounds with high anticancer activity and/or selectivity levels were selected. Some SAR aspects were determined and structure design directions were proposed.