- N-phenyl-2-pyrimidine-amine derivatives and process for the preparation thereof
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The present invention relates to an N-phenyl-2-pyrimidine-amine derivative showing a superior effect on lung cancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer, breast cancer, chronic or acute leukemia, hematologic malignancy, encephalophyma, bladder cancer, rectal cancer, or cervical cancer, etc. of warm-blooded animals and its salt. The present invention also relates to a process for preparing the compound, and to a pharmaceutical composition for the treatment of the above various diseases, which comprises an effective amount of the compound as an active ingredient together with pharmaceutically acceptable inert carriers.
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- N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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The present invention relates to an N-phenyl-2-pyrimidine-amine derivative showing a superior effect on tumor, lung cancer, gastric cancer, etc. of warm-blooded animals and its salt. The present invention also relates to a process for preparing the compound and a pharmaceutical composition for the prevention and treatment of such diseases as tumor, lung cancer, gastric cancer, etc., which comprises the compound as an active ingredient.
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- N-PHENYL-2-PYRIMIDINE-AMINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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The present invention relates to an N-Phenyl-2-pyrimidine-aminine derivative showing a superior effect on lung cancer, gastric cancer, colon cancer, pancreatic cancer, hepatoma, prostatic cancer, breast cancer, chronic or accute leukemia, hematologic malignancy, encephalophyma, bladder cancer, rectal cancer or cervical cancer, etc. of warm blooded animals and its salt. The present invention also relates to a process for preparing the compound, and to a pharmaceutical composition for the treatment of the above various disease, which comprises an effective amount of the compound as an active ingredient together with pharmaceutically acceptable inert carriers.
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- 2-Anilino-4-(thiazol-5-yl)pyrimidine CDK Inhibitors: Synthesis, SAR Analysis, X-ray Crystallography, and Biological Activity
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Following the identification through virtual screening of 4-(2,4-dimethyl-thiazol-5-yl)pyrimidin-2-ylamines as moderately potent inhibitors of cyclin-dependent kinase-2 (CDK2), a CDK inhibitor analogue program was initiated. The first aims were to optimize potency and to evaluate the cellular mode of action of lead candidate molecules. Here the synthetic chemistry, the structure-guided design approach, and the structure-activity relationships (SARs) that led to the discovery of 2-anilino-4-(thiazol-5-yl)pyrimidine ATP-antagonistic CDK2 inhibitors, many with very low nM Kis against CDK2, are reported. Furthermore, X-ray crystal structures of four representative analogues from our chemical series in complex with CDK2 are presented, and these structures are used to rationalize the observed biochemical SARs. Finally results are reported that show, using the most potent CDK2 inhibitor compound from the current series, that the observed antiproliferative and proapoptotic effects are consistent with cellular CDK2 and CDK9 inhibition.
- Wang, Shudong,Meades, Christopher,Wood, Gavin,Osnowski, Andrew,Anderson, Sian,Yuill, Rhoda,Thomas, Mark,Mezna, Mokdad,Jackson, Wayne,Midgley, Carol,Griffiths, Gary,Fleming, Ian,Green, Simon,McNae, Iain,Wu, Su-Ying,McInnes, Campbell,Zheleva, Daniella,Walkinshaw, Malcolm D.,Fischer, Peter M.
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p. 1662 - 1675
(2007/10/03)
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- Anti-cancer compounds
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The present invention relates to 2-substituted 4-heteroaryl-pyrimidines, their preparation, pharmaceutical compositions containing them and their use as inhibitors of cyclin-dependent kinases (CDKs) and hence their use in the treatment of proliferative disorders such as cancer, leukaemia, psoriasis and the like.
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- PYRIMIDINE DERIVATIVES AND PROCESSES FOR THE PREPARATION THEREOF
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There are described N-phenyl-2-pyrimidine-amine derivatives of formula I wherein R1 is 4-pyrazinyl, 1-methyl-1H-pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each case is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstituted or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen, R2, R3, R9, X, Y, n and R10 are defined in claim 1 These compounds can be used, for example, in the therapy of tumoral diseases.There are described N-phenyl-2-pyrimidine-amine derivatives of formula I (I) wherein R1 is 4-pyrazinyl, 1-methyl-1H-pyrrolyl, amino- or amino-lower alkyl-substituted phenyl wherein the amino group in each case is free, alkylated or acylated, 1H-indolyl or 1H-imidazolyl bonded at a five-membered ring carbon atom, or unsubstituted or lower alkyl-substituted pyridyl bonded at a ring carbon atom and unsubstituted or substituted at the nitrogen atom by oxygen, R2, R3, R9, X, Y, n and R10 are defined in claim 1. These compounds can be used, for example, in the therapy of tumoral diseases.
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- N-PHENYL-N,N"-GUANIDINEDICARBOXYLIC ACID ESTERS. SYNTHESIS, ANTHELMINTIC AND PESTICIDAL EFFECTS
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Substituted phenylammonium chlorides react with cyanamide to give the corresponding phenylguanidines which on treatment with chloroformate esters give N-subst.phenyl-N,N''-guanidinedicarboxylic acid esters.All substances prepared have been tested for their anthelmintic activity against the model helminths Nippostrongylus brasiliensis and Hymenolepis nana var. fraterna.The most significant activity has been found with diethyl N-(4-nitrophenyl)-N,N''-guanidinedicarboxylate.In pesticidal screening the compounds have shown fungicidal activity and particularly ovicidal activity against Tetranychus urticae which activity is increased with the compounds having a nitro group in the benzene ring.
- Palat, Karel,Celadnik, Milan,Danek, Jaroslav,Varkonda, Stefan
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p. 1127 - 1133
(2007/10/02)
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