[Synthesis and pharmacologic evaluation of 3-(2- and 4-pyridinyl)indane-1,3-diones and structural analogues with potential anti-inflammatory and antineoplastic activity].
Our on going work in the series of enamido-diketones issued from 2-azaarylindane-1,3-diones led us to synthesize and experiment N and C2-substituted derivatives of 2-(2 and 4-pyridinyl)indane-1,3-diones as well as of structurally related compounds resulting from the replacement of pyridine by quinoline and benzimidazole. Pharmacological evaluation of their anti-inflammatory activity (by inhibition of carrageenan foot edema) and their anticoagulant activity (by prothombin assay) led to the conclusion of the possibility of achieving a selective anti-inflammatory effect. It has been previously established that anticoagulants are liable to exert a protective effect in the development of cancer metastasis. Nevertheless none of the six experimented 2-(pyridin-2-yl)indane-1,3-diones extended survival time of mice treated by P388 lymphocytic leukemia.
Robert-Piessard
S
S
Laboratoires de Chimie Organique et de Chimie Thérapeutique, UFR des Sciences Pharmaceutiques, Nantes.
Leblois
D
D
Courant
J
J
Le Baut
G
G
Petit
J Y
JY
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000138:chemical synthesis* / Q000494:pharmacology; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000494:pharmacology; D055598:Chemical Phenomena; D002627:Chemistry, Physical; D005260:Female; D007189:Indans / Q000138:chemical synthesis* / Q000494:pharmacology; D008297:Male; D051379:Mice; D008811:Mice, Inbred DBA; D008815:Mice, Inbred Strains; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology; D051381:Rats
D000894:Anti-Inflammatory Agents, Non-Steroidal; D000970:Antineoplastic Agents; D007189:Indans; D011725:Pyridines
Synthèse et évaluation pharmacologique de 2-(2 et-4-pyridinyl)indane-1,3-diones et d'analogues structuraux à potentialités anti-inflammatoire et antitumorale.