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New derivatives of 2,7‐naphthyridine‐3‐carboxylic acid were synthesized. We report the hydrolysis, chlorination, alkylation, and amination of the 2,7‐naphthyridine esters 1, 2. A series of Schiff's bases 8a, 8b, 8c, 8d, 8e, 8f, 8g, 8h, 8i, 8j, 9a, 9b, 9b', 9c, 9d, 9e were produced by treating the obtained hydrazides 6 and 7 with aromatic aldehydes. The anticancer activities of the obtained derivatives were examined. Eighteen of the 24 newly synthesized compounds were qualified by the National Cancer Institute NCI (Bethesda, MD, USA) for in vitro screening against 60 different human tumor cell lines. The most active compound 8i was evaluated against a 60‐cell panel at five concentration levels and proved to be most sensitive towards central nervous system cancer (SF‐539), with GI50 = 0.70 µmol, total growth inhibition = 5.41 µmol, and LC50 = 53.7 µmol.

A series of new derivatives of 3-phenylthiazolo[4,5-d]pyrimidine-2-thiones were synthesized by the cyclization of 4-amino-5-alkyl(aryl) carboxamido-2,3-dihydrothiazolo-2-thione with aromatic aldehydes. Amine moieties were substituted in position 7 of the obtained bicyclic compounds. The synthesized compounds were characterized by elemental analysis, IR, 1H-NMR, and 13C-NMR spectral data. Some of the newly synthesized compounds were selected by the U.S. National Cancer Institute for in vitro antitumor screening. The two compounds 3d 7-chloro-5-(4-fluorophenyl)-3-phenyl-4,5-dihydro-3H-thiazolo[4,5-d]pyrinimidine-2-thione and 4i 5-(2-chlorophenyl)-7-(4-fluorobenzylaxnlno)-3-phenyl-4,5-dihydro-3H-thiazolo[4,5-dipyrhflldlfle-2thione proved to be the most active in the present study and their antitumor activities against 60 human tumor cell lines were described.

Fused pyridine derivatives R 0450 Synthesis, Structure, and Pharmacological Screening of 2,7-Naphthyridine Derivatives. -A method for the rearrangement of pyrrolo[3,4-c]pyridines (III) and (VI) into the corresponding 2,7-naphthyridines is developed. Derivative (IV) demonstrates growth inhibition of the ovarian cancer cell line IGROV1. -(WAGNER*, E.; WOJCICKA, A.; BRYNDAL, I.; LIS, T.; Pol.

Isoxazole derivativesIsoxazole derivatives R 0240 Synthesis and Cytostatic Activity of 4-Substituted Derivatives of Isoxazolyltriazenes. -Novel analogues of Dacarbazin, a clinically used triazene active against L1210 leukaemia and malignant melanoma, are synthesized from diazonium salt (II). Triazenoisoxazoles (IVa) and (IVc) show cytostatic activity similar to Dacarbazin. -(WAGNER, E.; OPOLSKI, A.; WIETRZYK, J.; Pol.

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A number of derivatives of isoxazolo [4,3-d]pyrimidine and isoxazolo [4,5-d]pyrimidine were prepared with potential anticancer activity. Condensation of 4-amino-5-benzoyl-isoxazolo-3-carboxylic acid hydrazide with ethyl orthoformate and then with different amines gave a series of 3-benzoyl-7-oxo-7H-isoxazolo[4,3-d]pyrimidin-6-yl-aryliden-formamidine. A series of 5-aminomethyl-7-phenyl-isoxazolo[4,5-d]pyrimidine-3-carboxamide was obtained from 4-amino-5-benzoylisoxazole-3-carboxamide with acetonitrile, and chloroacetonitrile with gaseous hydrogen chloride. Some of these compounds were tested for their cytotoxic activity.