- Efficient synthesis and biological evaluation of proximicins A, B and C
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A quick and efficient synthesis and the biological evaluation of promising antitumor-antibiotics proximicins A, B and C are reported. The characteristic repetitive unit of these molecules, the methyl 4-Boc-aminofuran-2-carboxylate 15, was prepared in thre
- Brucoli, Federico,Natoli, Antonino,Marimuthu, Preethi,Borrello, Maria Teresa,Stapleton, Paul,Gibbons, Simon,Sch?tzlein, Andreas
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experimental part
p. 2019 - 2024
(2012/05/05)
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- Disubstituted aryl and heteroaryl imines having retinoid-like biological activity
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Compounds of the formula STR1 wherein the R 1 groups independently are hydrogen, lower alkyl, or two geminal R 1 groups jointly represent an oxo ( O) or a thio ( S) group; R 2 is hydrogen or lower alkyl, or halogen; M is or --N CR 4 -- or --R 4 C N-- where R 4 is hydrogen or lower alkyl; X is C(R 1) 2 ; Y is phenyl optionally substituted with an R 3 group which is lower alkyl or halogen; A is (CH 2) n where n is 0-5, lower branched chain alkyl, cycloalkyl, alkenyl, alkynyl; B is hydrogen, COOH or a pharmaceutically acceptable salt thereof, COOR 8, CONR 9 R 10, --CH 2 OH, CH 2OR 11, CH 2 OCOR 11, CHO, CH(OR 12) 2, CHOR 13 O, --COR 7, CR 7 (OR 12) 2, or CR 7 OR 13 O, where R 7 is an alkyl, cycloalkyl or alkenyl group containing 1 to 5 carbons, R 8 is an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5 to 10 carbons, or R 8 is phenyl or lower alkylphenyl, R 9 and R 10 independently are hydrogen, an alkyl group of 1 to 10 carbons, or a cycloalkyl group of 5-10 carbons, or phenyl or lower alkylphenyl, R 11 is lower alkyl, phenyl or lower alkylphenyl, R 12 is lower alkyl, and R 13 is divalent alkyl radical of 2-5 carbons have retinoid-like biological activity.
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