- Design and synthesis of DNA-intercalative naphthalimide-benzothiazole/cinnamide derivatives: cytotoxicity evaluation and topoisomerase-IIα inhibition
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A new series of different naphthalimide-benzothiazole/cinnamide derivatives were designed, synthesized and tested for their in vitro cytotoxicity on selected human cancer cell lines. Among them, derivatives 4a and 4b with the 6-aminobenzothiazole ring and 5g with the cinnamide ring displayed potent cytotoxic activity against colon (IC50: 3.715 and 3.467 μM) and lung cancer (IC50: 4.074 and 3.890 μM) cell lines when compared to amonafide (IC50: 5.459 and 7.762 μM). Later, the DNA binding studies for these selected derivatives (by CD, UV/vis, fluorescence spectroscopy, DNA viscosity, and molecular docking) suggested that these new derivatives significantly intercalate between two strands of DNA. In addition, the most potent derivatives 4a and 4b were also found to inhibit DNA topoisomerase-II.
- Sankara Rao,Nagesh, Narayana,Lakshma Nayak,Sunkari, Satish,Tokala, Ramya,Kiranmai, Gaddam,Regur, Phanindranath,Shankaraiah, Nagula,Kamal, Ahmed
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- A phenyl [...] hERG potassium ion channel of small molecule fluorescent probe and its application (by machine translation)
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The invention discloses a phenyl furan small molecule fluorescent probe and its application. The general structure of the fluorescent probe shown in formula (I): In the formula, R 1 is halogen, a mono-substituted alkyl or alkoxy substituent base or many ; R 2 to fluorophore; n=1-6 ; ethylene in between with the fluorophore containing 1-6 is connected with the carbon of the alkyl chain. The fluorescence probe molecule can be used to mark hERG potassium ion channel, can be used for hERG the activity of the potassium ion channel inhibitors screening and listing pharmaceutical evaluation of the cardiac toxicity, in addition can also as a tool to medicine hERG potassium ion channel related phannacological, pathology and physiol research. Furthermore, this kind of compound preparation method mild reaction conditions, the raw material is cheap and easy to obtain, operation and after treatment is simple. (by machine translation)
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Paragraph 0057; 0081
(2016/11/24)
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- Remarkable DNA binding affinity and potential anticancer activity of pyrrolo[2,1-c][1,4]benzodiazepine-naphthalimide conjugates linked through piperazine side-armed alkane spacers
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A series of pyrrolobenzodiazepine-naphthalimide conjugates tethered through a piperazine ring system have been designed, synthesized, and evaluated for their anticancer activity. These new conjugates exhibit very high DNA binding affinity and cytotoxic ac
- Kamal, Ahmed,Ramu,Tekumalla, Venkatesh,Ramesh Khanna,Barkume, Madan S.,Juvekar, Aarti S.,Zingde, Surekha M.
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p. 7218 - 7224
(2008/12/22)
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- Various 2-(substituted piperazinyl)-1H-benz [de]isoquinoline-1,3 (2H) -diones
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Compounds of the following formula and their acid addition salts STR1 Z is STR2 A is straight or branched chain alkylene of 2 to 6 carbons; B is straight chain alkylene of 2 to 4 carbons; X is straight or branched chain alkyl of 1 to 8 carbons, phenyl, benzyl, phenethyl, substituted phenyl, substituted benzyl, or substituted phenethyl, R1 and R2 are located at the 7 or 8 and 5 or 6 position respectively and are independently selected from the group consisting of hydrogen, straight or branched chain alkyl of 1 to 4 carbons, straight or branched chain alkoxy of 1 to 4 carbons, Cl, Br, F, amino, nitro, CF3, and cyano; are disclosed. These compounds possess antiprotozoal activity.
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