Banyu Pharmaceutical Co. Ltd

Katsuhisa Kojiri

Hiroyuki Suda

Hisao Kondo

Mitsuru Ohkubo

Hiroharu Arakawa

Hajime Suzuki

Masao Nagashima

Seiichi Tanaka

Shigeru Nakajima

Masanori Okanishi

Hidenori Ogawa

Akira Okura

Daisuke Uemura

Atsushi Hirano

Kohtaro Funaishi

Hiromasa Okada

Kenji Kawamura

Eiji Sugiyama

Aisaku Fuse

Koichiro Torigoe

Hiroshi Kushida

Shigeru Uchiyama

Seigou Kamiya

Seigo Kamiya

Indolopyrrolocarbazole derivatives and antitumor agents

A compound represented by the formula &lsqb;I&rsqb;

Sesterterpene derivatives exhibiting antifungal activities

This invention relates to glycosyltransferase, genes encoding glycosyltransferase, recombinant vectors having such a gene, host cells transformed with such a recombinant vector, and uses thereof. This invention makes it possible to glycosylate indolopyrrolocarbazole derivatives conveniently and economically.

Gene encoding glycosyltransferase and its uses

Derivatives of antifungal substance BE-31405 and process for producing

Antifungal substances BE-49385 and process for their production

Antifungal composition

This invention relates to compounds of the general formula ##STR1## or pharmaceutically salts thereof, wherein R.sup.1 and R.sup.2 each represent an OH group, R.sup.1 is located at the 1- or 2-position, R.sup.2 is located at the 10- or 11-position, R.sup.2 is located at the 11-position when R.sup.1 is located at the 1-position, and R.sup.2 is located at the 10-position when R.sup.1 is located at the 2-position. The compounds of the present invention have an excellent antitumor effect and are hence useful as antitumor agents in the field of medicine.

Antitumor indolopyrrolocarbazole derivatives

Indolopyrrocarbazole derivatives represented by formula (I) and the pharmaceutically acceptable salts thereof have excellent antitumor activity as evidenced by their in vitro proliferation inhibiting activity against mouse leukemia cell, human gastric cancer cell, human lung cancer cell and human colon cancer cell, ##STR1## wherein R.sup.1 and R.sup.2 independently represent, for example, a hydrogen atom or various hydrocarbon groups which may be substituted or heterocyclic groups which may also be substituted; or a group --Y--R.sup.3 where Y represents a carbonyl group, thiocarbonyl group or sulfonyl group and R.sup.3 represents a hydrogen atom or one of various aliphatic, cycloaliphatic, aryl, nitrogen-containing (e.g. amino, hydrazino, etc) or heterocyclic groups, which groups may be substituted by various substituents; or R.sup.1 and R.sup.2 may combine to represent a lower alkylidene group which may be substituted; or R.sup.1 and R.sup.2, together with the N-atom to which they are bonded form a heterocyclic group which may be substituted; G represents a pentose or hexose group; and X.sup.1 and X.sup.2, independently, represent, for example, hydrogen, halogen, amino, hydroxyl, alkoxy, aryloxy, carboxyl, alkoxycarbonyl or alkyl. These compounds have improved water solubility as compared to rebeccamycin.

Indolopyrrolocarbazole derivatives

Indolopyrrolocarbazole derivatives, such as, for example, 12,13-dihydro-1,11-dihydroxy-13-(.beta.-D-glucopyranosyl)-5H-indolo[2,3-a] pyrrolo[3,4-c]carbazole-5,7-(6H)-dione or 6-amino derivative thereof, are produced by glycosylating a precursor compound by cultivating with Microtetraspora sp. A34549, Saccharothrix aerocolonigenes ATCC 39243 or mutants thereof, in a nutrient medium containing the precursor compound.

Microbial process for preparation of indolopyrrolocarbazole derivatives

Indolopyrrocarbazole derivatives such as exemplified by the following compound, ##STR1## have excellent antitumor activity as evidenced by in vitro proliferation inhibiting activity against mouse leukemia cell, human gastric cancer cell, human lung cancer cell and human colon cancer cell.

A compound of formula (VIII) ##STR1## is added to a culture media containing Microtetraspora sp. A34549 or Saccharothrix aerocolonigenes ATCC 39243. The compound is glycosylated to form an indolopyrrolocarbazole of formula (VII) ##STR2##

Process for producing glycosylated indolopyrrolocarbazole derivatives by

This invention relates to 12,13-dihydro-6H-indolo[2,3-a]pyrrolo[3,4-c]carbazole-5,7(6H)-dione derivatives represented by the following general formula, pharmaceutically acceptable salts thereof, a method for preparation thereof and a use thereof: ##STR1## [wherein R.sup.1 denotes a monosaccharide group having 5 to 7 carbon atoms, and the hydroxyl groups of this monosaccharide group can be replaced by the same or different 1 to 3 groups selected from the group consisting of a hydrogen atom, lower alkyl group, lower alkylcarbonyloxy group and lower alkoxy group.]

Method for preparing antitumor substance BE-13793C derivatives

Antitumor substance BE-13793C derivatives

Growing community of inventors

Tsukuba, Japan

Katsuhisa Kojiri