Antitumor activity of asterriquinones from Aspergillus fungi. IV. An attempt to modify the structure of asterriquinones to increase the activity. | Zendy

Sakae Shimizu | Zendy; Yuzuru Yamamoto | Zendy; Shunichi Koshimura | Zendy

Open Access

Antitumor activity of asterriquinones from Aspergillus fungi. IV. An attempt to modify the structure of asterriquinones to increase the activity.

Author(s) -

Sakae Shimizu,

Yuzuru Yamamoto,

Shunichi Koshimura

Publication year - 1982

Publication title -

chemical and pharmaceutical bulletin

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.393

H-Index - 92

eISSN - 1347-5223

pISSN - 0009-2363

DOI - 10.1248/cpb.30.1896

Subject(s) - chemistry , in vivo , biological activity , stereochemistry , structure–activity relationship , chemical structure , chemical modification , active compound , aspergillus , in vitro , biochemistry , organic chemistry , microbiology and biotechnology , biology

An attempt was made to obtain more potent antitumor compounds by chemically modifying asterriquinones. Amino-and aziridinyl-asterriquinone were newly synthesized, but showed no activity. However, dimethylallylation of asterriquinone Cl, which had no effect in vivo, yielded an active compound, with a change in pKa value from 5.0 to 7.2. This suggests that other active compounds may be obtained by the chemical modification of asterriquinones with various other functional groups

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