Biologically Active Heteroarotinoids Exhibiting Anticancer Activity and Decreased Toxicity

• Published in: Journal of medicinal chemistry Vol. 40; no. 22; pp. 3567 - 3583
• Main Authors: Benbrook, Doris M, Madler, Matora M, Spruce, Lyle W, Birckbichler, Paul J, Nelson, Eldon C, Subramanian, Shankar, Weerasekare, G. Mahika, Gale, Jonathan B, Patterson, Manford K, Wang, Binghe, Wang, Wei, Lu, Shennan, Rowland, Tami C, DiSivestro, Paul, Lindamood, Charles, Hill, Donald L, Berlin, K. Darrell
• Format: Journal Article
• Language: English
• Published: WASHINGTON American Chemical Society 24.10.1997; Amer Chemical Soc
• Subjects: Animals; Antineoplastic agents; Antineoplastic Agents - chemistry; Antineoplastic Agents - pharmacology; Antineoplastic Agents - toxicity; Biological and medical sciences; Cell Division - drug effects; Chemistry, Medicinal; General aspects; Humans; Life Sciences & Biomedicine; Magnetic Resonance Spectroscopy; Male; Mass Spectrometry; Medical sciences; Mice; Molecular Structure; Pharmacology & Pharmacy; Pharmacology. Drug treatments; Retinoids - chemistry; Retinoids - pharmacology; Retinoids - toxicity; Science & Technology; Tumor Cells, Cultured; GENE-EXPRESSION; F9 TERATOCARCINOMA CELLS; 13-CIS-RETINOIC ACID; RETINOID-X-RECEPTOR; TERMINAL DIFFERENTIATION; INDUCTION; TISSUE TRANSGLUTAMINASE; CARCINOMA; VITAMIN-A; ACUTE PROMYELOCYTIC LEUKEMIA; Antineoplastic agent; Toxicity; Cytotoxicity; Male; Retinoids; Oxygen heterocycle; Chroman derivatives; Hypervitaminosis; Structure activity relation; Carboxylic acid; Established cell line; Bicyclic compound; Aromatic compound; Chemical synthesis; Tumor cell; Human; Conjugated polyenic compound; Aliphatic compound; Rodentia; In vitro; In vivo; Vertebrata; Sulfur heterocycle; Mammalia; Mouse; Animal

A series of retinoids, containing heteroatoms in a cyclic ring and called heteroarotinoids, were synthesized, and their biological activity was evaluated using tissue culture lines that have measurable responses to trans-retinoic acid (t-RA). Transglutaminase (TGase) was assessed in the human erythr...