Cyclopenta[g]quinazoline-based antifolates: the effect of the chirality at the 6-position on the inhibition of thymidylate synthase (TS). |
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| Authors: | V Bavetsias J H Marriott D S Theti J C Melin S C Wilson A L Jackman |
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| Institution: | CRC Centre for Cancer Therapeutics at The Institute of Cancer Research, Chemistry Department, CRC Laboratory, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK. vassilio@icr.ac.uk |
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| Abstract: | Cyclopentag]quinazoline-based inhibitors of thymidylate synthase (TS) possess a chiral centre at the 6-position of the molecule. The effect of this chirality on the inhibition of TS was investigated by synthesising compounds 6S-1a-c, 6R-1a-c. It was shown, in particular with the diastereoisomers 6S-1c, 6R-1c, that the inhibitory activity against TS is mainly due to the 6S diastereoisomer rather than the 6R diastereoisomer, which is virtually inactive. |
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