INDOLOPYRROLOCARBAZOLE DERIVATIVES OF SUGARS, PHARMACEUTICAL COMPOSITION CONTAINING THEREOF AND METHOD OF INHIBITION OF TUMOR PROLIFERATION Russian patent published in 2001 - IPC

Abstract RU 2167880 C2

FIELD: organic chemistry, pharmacy. SUBSTANCE: invention relates to novel indolopyrrolocarbazole derivatives of sugars of the general formula (I) where one of R1 and R1a means hydrogen atom but other is not hydrogen atom; R2 and mean independently hydrogen atom, OH; R3 and mean independently hydrogen atom, OH; R4 and mean independently hydrogen atom, OH, azido-group, NH2, halogen atom; mean independently H, OH, azido-group, NR9R10, halogen atom, C(O)Ra, SR, OSO2Rc, OR or in common they form =O under condition that R2,R3,R4,R5 and and all are not hydrogen atom simultaneously; R means hydrogen atom, C1-7-alkyl, heterocyclic 6-membered ring containing 1 or 2 nitrogen atoms as heteroatoms being indicated C1-7-alkyl can be substituted with phenyl; Ra means OH; Rc means C1-7-alkyl; R6 means hydrogen atom, C1-7-alkyl, OH, NH2 being indicated C1-7-alkyl can be substituted with phenyl which in turn can be substituted with C1-7-alkyl; R7 and R8 in common mean O; R9 and R10 mean independently hydrogen atom or in common with nitrogen atom to which they are bound form cyclic 6-membered nonaromatic ring containing one or two heteroatoms taken among the group N, O; and mean independently H, halogen atom, -C(O)Ra under condition that and are not 1,11-dichloro-group and under condition that when X2 and each means H, X1 and then each means independently H or halogen atom; R1 means hexose; R7 and R8 in common mean O and each of R2,R5 and R4 means OH; and each means H; Q means NH and in this case each of R3 and R6 is not NH2 and R3 is not methoxy-group when R6 means H; W means C; Q means NH, O or S; or its pharmaceutically acceptable salt. Compounds of the formula (I) show activity with respect to topoisomerase-1 and can be used for inhibition of proliferation of tumor cells eliciting antitumor effect. Invention describes pharmaceutical composition and method of inhibition of tumor growth also. EFFECT: new compounds, valuable antitumor activity. 18 cl, 3 tbl, 106 ex

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RU 2 167 880 C2

Authors

Sauln'Er Mark Georg

Behlasubraman'Jan Nilakantan

Frennesson Dehvid Bertil

St. Loran Denis R.

Lehngli Dehvid R.

Dates

2001-05-27Published

1997-08-21Filed