60811-24-7Relevant articles and documents
Highly convergent synthesis of a rebeccamycin analog with benzothioeno(2,3-a)pyrrolo(3,4-c)carbazole as the aglycone
Wang, Jianji,Soundarajan, Nachimuthu,Liu, Nian,Zimmermann, Kurt,Naidu, B. Narasimhulu
, p. 907 - 910 (2007/10/03)
A highly convergent, scalable synthesis of the rebeccamycin analog 2 was demonstrated in seven steps and 31% overall yield based on the N-protected building block dibromomaleimide 7. The practical synthesis of other two building blocks, 5,6-difluoro-3-ben
Novel 2-amino-4-oxo-5-arylthio-substituted-pyrrolo[2,3-d]pyrimidines as nonclassical antifolate inhibitors of thymidylate synthase
Gangjee, Aleem,Jain, Hiteshkumar D.,Kisliuk, Roy L.
, p. 2225 - 2230 (2007/10/03)
A series of 17 novel 2-amino-4-oxo-5-[(substituted phenyl)thio]pyrrolo[2,3- d]pyrimidines were synthesized as potential inhibitors of thymidylate synthase (TS) and as antitumor agents. The analogues contain a variety of electron withdrawing substituents on the phenyl ring of the side chain and were evaluated as inhibitors of human TS (hTS) and Escherichia coli TS and of human and E. coli dihydrofolate reductase (DHFR). The analogues 14, 17, and 18 were potent inhibitors of hTS with IC50 values of 0.28, 0.21, and 0.22 μM, respectively, and were more potent than the clinically used ZD1694, 2 and LY231514, 3 against human TS.
Use of compounds for the elevation of pyruvate dehydrogenase activity
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, (2008/06/13)
The use of compounds of the formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs: wherein: Ring C is phenyl or a carbon linked heteroaryl ring substituted as defmed within; R1is an ortho substituent as defined within; n is 1 or 2; A—B is a linking group as defined within; R2and R3are as defined within; R4is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are also described.
Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine
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, (2008/06/13)
Polysubstituted derivatives of 10-piperazinodibenzo (b,f) thiepine and processes for the preparation thereof are described. The compositions evidence psychotropic and antimicrobial characteristics and are of low toxicity. The described compounds are of the general formula STR1 wherein R2, R3, R7 and R8 are selected from among hydrogen, fluorine and chlorine atoms, a fluoromethyl group, a methoxy group and a hydroxyl group, at least three of R2, R3, R7 and R8 being other than hydrogen, R being selected from among hydrogen, alkyl or alkylhydroxy groups having from 1-3 carbon atoms, an acyloxyalkyl group having from 8-10 carbon atoms in the acyl moiety and from 2-3 carbon atoms in the alkyl moiety and an ethoxycarbonyl group, m and n representing integers from 0-1 and the bond between the 10 and 11 carbon atoms being either a single or double bond.