Tumor localizing agents III Radioiodinated quinoline derivatives

Counsell, Raymond E.; Pocha, P.; Morales, José O.; Beierwaltes, William H.

doi:10.1002/jps.2600560835

Cited by 15 publications

(1 citation statement)

References 5 publications

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“…Among them, 4-(3-dimethylaminopropylamino)-7-[125I]iodoquinoline was shown to concentrate in malignant melanoma of mice, Syrian hamsters, dogs, and man. 31,32 Recently, Adamson33 has suggested that alkylating agents be designed utilizing carriers that are most likely to deliver the agents to specific target sites. He further suggested that by designing drugs with activity against specific types of tumors rather than with generalized cytotoxic agents, it should be possible to increase the therapeutic index of these agents.…”

Section: -(33-dimethyl-l-triazeno)quinolinesmentioning

confidence: 99%

Synthesis and antitumor activity of halogen-substituted 4-(3,3-dimethyl-1-triazeno)quinolines

Lin¹,

Loo²

1978

J. Med. Chem.

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Halogenated 4-(3,3-dimethyl-1-triazeno)quinolines were synthesized as potential antitumor agents on the basis of the biochemical pharmacological properties of existing triazenes, their structural-activity relationships, and the high melanin binding of chloroquine and iodoquine in vivo and in vitro. They were synthesized by diazotization of appropriate halogen-substituted 4-aminoquinolines in fluoboric acid at -5 degrees C followed by coupling with dimethylamine. Among these new compounds, 8-chloro-4-(3,3-dimethyl-1-triazeno)quinoline produces significant antitumor activity against both P-388 and L1210 murine leukemias. Although only marginally active or inactive against P-388, the other chloro, bromo, or iodo analogues show activity against L1210 comparable to that of dacarbazine (DIC). However, none of these compounds is active against B-16 melanoma. Compared with DIC these new agents demonstrate a higher in vitro affinity for melanin; however, this affinity is apparently not correlated with their antitumor activity.

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Section: -(33-dimethyl-l-triazeno)quinolinesmentioning

confidence: 99%