- Scaffold-hopping strategy: Synthesis and biological evaluation of 5,6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents
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Utilizing scaffold-hopping drug-design strategy, we sought to identify a backup drug candidate for BPR0L075 (1), an indole-based anticancer agent. For this purpose, 5,6-fused bicyclic heteroaromatic scaffolds were designed and synthesized through shufflin
- Tung, Yen-Shih,Coumar, Mohane Selvaraj,Wu, Yu-Shan,Shiao, Hui-Yi,Chang, Jang-Yang,Liou, Jing-Ping,Shukla, Paritosh,Chang, Chun-Wei,Chang, Chi-Yen,Kuo, Ching-Chuan,Yeh, Teng-Kuang,Lin, Chin-Yu,Wu, Jian-Sung,Wu, Su-Ying,Liao, Chun-Chen,Hsieh, Hsing-Pang
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supporting information; scheme or table
p. 3076 - 3080
(2011/06/25)
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- COMPOUNDS AND METHODS FOR KINASE MODULATION, AND INDICATIONS THEREFOR
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Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof derivatives thereof, forms thereof are active on at least one Raf protein kinase. Also described are methods of use thereof to treat diseases and conditions, including diseases and conditions associated with activity of Raf protein kinases, including melanoma, colorectal cancer, thyroid cancer, ovarian cancer, cholangiocarcinoma, pain or polycystic kidney disease.
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Page/Page column 32
(2009/12/05)
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- Anti-tumor compounds
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Compounds of the following formula: wherein A, D, Q, T, U, V, W, X, Y, Z, R1, and ---- are as defined herein. This invention also relates to a method of inhibiting tubulin polymerization, or treating cancer or an angiogenesis-related disorder w
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Page/Page column 13; 14
(2008/06/13)
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- PPAR ACTIVE COMPOUNDS
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Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
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- Synthesis of 2'-deoxyisoinosine and related 2'-deoxyribonucleosides
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Various 2-substituted purine and pyrrolo[2,3-d]pyrimidine 2'-deoxyribonucleosides with methylthio (13a), chloro (13b), methoxy (9b), and oxo (2, 3) substituents at C(2) are prepared. They are obtained either via stereoselective nucleobase-anion glycosylation or by base transformation. A three-step synthesis of the unknown 2'-deoxyisoinosine (2) from 2'-deoxyguanosine (15) is described. Compound 2 as well as its 7-deazapurine derivative 3 exhibit strong fluorescence.
- Seela,Chen,Bindig,Kazimierczuk
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p. 194 - 202
(2007/10/02)
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- Condensed heteroaromatic ring systems. XXI. Synthesis of pyrrolo[2,3-d]pyrimidines and pyrrolo[3,2-d]pyrimidines
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Pyrrolo[2,3-d]pyrimidines and pyrrolo[3,2-d]pyrimidines were synthesized in high yields by the palladium-catalyzed reaction of 4-acetylamino-5-bromopyrimidines and 5-acetylamino-4-iodopyrimidines with (Z)-1-ethoxy-2-(tributylstannyl)ethene followed by cyclization under acidic conditions.
- Sakamoto,Satoh,Kondo,Yamanaka
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