Antitumor activity of benzo[a]phenothiazines.
We have previously reported on the diverse biological activities of benzo[a]phenothiazines, such as the induction of antitumor and antimutagenic activity in vivo, and differentiation and apoptosis in vitro. The relationship of radical generation and pi-spin density or dipole moment was investigated, using quantum-chemical calculation with UHF/PM3. These data suggest that the origin of radical generation by active benzo[a]phenothiazines, which affect such biological activities might be N-atom at position 12.
Motohashi
N
N
Meiji Pharmaceutical University, Tokyo, Japan.
Kurihara
T
T
Satoh
K
K
Sakagami
H
H
Mucsi
I
I
Pusztai
R
R
Szabó
M
M
Molnár
J
J
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1 / Q000037:antagonists & inhibitors; D000818:Animals; D000951:Antigens, Neoplasm / Q000096:biosynthesis / Q000235:genetics; D000970:Antineoplastic Agents / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D017209:Apoptosis / Q000187:drug effects; D001205:Ascorbic Acid / Q000737:chemistry; D001692:Biological Transport / Q000187:drug effects; D002286:Carcinoma, Ehrlich Tumor / Q000188:drug therapy / Q000473:pathology; D002454:Cell Differentiation / Q000187:drug effects; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D015195:Drug Design; D018432:Drug Resistance, Multiple; D019008:Drug Resistance, Neoplasm; D004354:Drug Screening Assays, Antitumor; D005609:Free Radicals; D015972:Gene Expression Regulation, Neoplastic / Q000187:drug effects; D006801:Humans; D015394:Molecular Structure; D009369:Neoplasms / Q000188:drug therapy / Q000276:immunology / Q000473:pathology; D009374:Neoplasms, Experimental / Q000188:drug therapy / Q000276:immunology / Q000473:pathology; D010640:Phenothiazines / Q000737:chemistry / Q000494:pharmacology / Q000627:therapeutic use*; D013329:Structure-Activity Relationship
D020168:ATP Binding Cassette Transporter, Subfamily B, Member 1; D000951:Antigens, Neoplasm; D000970:Antineoplastic Agents; D005609:Free Radicals; D010640:Phenothiazines; C107575:benzophenothiazine; D001205:Ascorbic Acid