- Evaluation of alkylating and intercalating properties of mannich bases for cytotoxic activity
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A series of new "hybrid compounds", Mannich base derivatives of planar polycyclic/heterocyclic starting materials, was designed and synthesized. The structures of the compounds were confirmed by spectroscopic methods and elemental analysis. Cytotoxicity of compounds was investigated in three cancer cell lines (PC3, HeLa, and MCF7) and one non-tumoral cell line (293 HEK). We tested the DNA-intercalating capability of the molecules by ethidium bromide (EtBr) fluorescence displacement experiment. Compounds' alkylation potency was investigated via in vitro incubation test using 2-mercaptoethanol, a biomimetic nucleophile. The five of the compounds (7s, 9d, 10b, 11b, 12c) are reported for first time in the literature. Our results suggest that compound 9d has a biological activity close to the reference compound doxorubicin, an intercalating agent in clinical use.
- Istanbullu, Huseyin,Erzurumlu, Yalcin,Kirmizibayrak, Petek Ballar,Erciyas, Ercin
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p. 1096 - 1106
(2015/04/14)
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- Mannich Bases of 4-Phenyl-3-buten-2-one: A New Class of Antiherpes Agent
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The morpholine Mannich base of 4-phenyl-3-buten-2-one was found to have activity in model infections of herpes simplex.The activity was essentially equivalent to that of disodium phosphonoacetate.This paper presents the biological activity and synthesis o
- Edwards, M.L.,Ritter, H.W.,Stemerick, D.M.,Stewart, K.T.
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p. 431 - 436
(2007/10/02)
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- 5-Phenyl-2,4-pentadien-1-amines and method for inhibiting prostaglandin dehydrogenase
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5-Phenyl-2,4-pentadien-1-amines and salts thereof are provided having the structure STR1 wherein R1 is hydrogen, lower alkyl, lower alkoxy, hydroxy, lower alkanoyloxy, nitro, cyano, amino, carboxy or lower alkoxycarbonyl, and R2 and R3 are the same or different and are hydrogen, lower alkyl, alkenyl-lower alkyl, aralkyl, and substituted lower alkyl. These compounds possess useful pharmceutical activites due to their ability to inhibit the prostaglandin-inactivating enzyme 15-α-hydroxyprostaglandin dehydrogenase.
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