Journal
MOLECULES
Volume 27, Issue 17, Pages -Publisher
MDPI
DOI: 10.3390/molecules27175578
Keywords
pyrroloisoquinolines; kinase inhibition
Funding
- Ligue Nationale Contre le Cancer
- ITMO Cancer Aviesan Cancer Plan
- Biogenouest
- Ministere de l'Enseignement Superieur et de la Recherche
- Regional Council of Brittany
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A new series of pyrazolo[3,4-g]isoquinoline derivatives, diverse in substitution at the 4- or 8-position, were synthesized and evaluated for their kinase inhibitory potency. The results showed that the introduction of a bromine atom at the 8-position had a negative effect on Haspin inhibition, while the introduction of an alkyl group at the 4-position led to a modification of the kinase inhibition profiles. Overall, the new pyrazolo[3,4-g]isoquinolines represent a novel family of kinase inhibitors with various selectivity profiles.
A new series of pyrazolo[3,4-g]isoquinoline derivatives, diversely substituted at the 4- or 8-position, were synthesized. The results of the kinase inhibitory potency study demonstrated that the introduction of a bromine atom at the 8-position was detrimental to Haspin inhibition, while the introduction of an alkyl group at the 4-position led to a modification of the kinase inhibition profiles. Altogether, the results obtained demonstrated that new pyrazolo[3,4-g]isoquinolines represent a novel family of kinase inhibitors with various selectivity profiles.
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