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Design, synthesis, ...
Design, synthesis, HER2 inhibition and anticancer evaluation of new substituted 1,5-dihydro-4,1-benzoxazepines
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- Cruz-Lopez, Olga (författare)
- Univ Granada, Fac Pharm, Dept Med & Organ Chem, Campus Cartuja S-N, Granada 18071, Spain.;Univ Granada, Biosanit Inst Granada Ibs GRANADA, SAS, Granada, Spain.
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- Ner, Matilde (författare)
- Univ Granada, Fac Pharm, Dept Med & Organ Chem, Campus Cartuja S-N, Granada 18071, Spain.
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- Nerin-Fonz, Francho (författare)
- Uppsala universitet,Institutionen för cell- och molekylärbiologi
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- Jimenez-Martinez, Yaiza (författare)
- Univ Granada, Biosanit Inst Granada Ibs GRANADA, SAS, Granada, Spain.;Univ Granada, Biopathol & Med Regenerat Inst, Granada, Spain.;Univ Granada, Dept Human Anat & Embryol, Excellence Res Unit Modeling Nat MNat, Granada, Spain.
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- Araripe, David (författare)
- Uppsala universitet,Institutionen för cell- och molekylärbiologi
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- Marchal, Juan A. (författare)
- Univ Granada, Biosanit Inst Granada Ibs GRANADA, SAS, Granada, Spain.;Univ Granada, Biopathol & Med Regenerat Inst, Granada, Spain.;Univ Granada, Dept Human Anat & Embryol, Excellence Res Unit Modeling Nat MNat, Granada, Spain.
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- Boulaiz, Houria (författare)
- Univ Granada, Biosanit Inst Granada Ibs GRANADA, SAS, Granada, Spain.;Univ Granada, Biopathol & Med Regenerat Inst, Granada, Spain.;Univ Granada, Dept Human Anat & Embryol, Excellence Res Unit Modeling Nat MNat, Granada, Spain.
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- Gutiérrez-de-Terán, Hugo (författare)
- Uppsala universitet,Beräkningsbiologi och bioinformatik
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- Campos, Joaquin M. (författare)
- Univ Granada, Fac Pharm, Dept Med & Organ Chem, Campus Cartuja S-N, Granada 18071, Spain.;Univ Granada, Biosanit Inst Granada Ibs GRANADA, SAS, Granada, Spain.
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- Conejo-Garcia, Ana (författare)
- Univ Granada, Fac Pharm, Dept Med & Organ Chem, Campus Cartuja S-N, Granada 18071, Spain.;Univ Granada, Biosanit Inst Granada Ibs GRANADA, SAS, Granada, Spain.
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Univ Granada, Fac Pharm, Dept Med & Organ Chem, Campus Cartuja S-N, Granada 18071, Spain;Univ Granada, Biosanit Inst Granada Ibs GRANADA, SAS, Granada, Spain. Univ Granada, Fac Pharm, Dept Med & Organ Chem, Campus Cartuja S-N, Granada 18071, Spain. (creator_code:org_t)
- 2021-07-12
- 2021
- Engelska.
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Ingår i: Journal of enzyme inhibition and medicinal chemistry (Print). - : Taylor & Francis. - 1475-6366 .- 1475-6374. ; 36:1, s. 1553-1563
- Relaterad länk:
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https://doi.org/10.1...
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https://uu.diva-port... (primary) (Raw object)
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https://www.tandfonl...
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https://urn.kb.se/re...
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https://doi.org/10.1...
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Abstract
Ämnesord
Stäng
- A series of 11 new substituted 1,5-dihydro-4,1-benzoxazepine derivatives was synthesised to study the influence of the methyl group in the 1-(benzenesulphonyl) moiety, the replacement of the purine by the benzotriazole bioisosteric analogue, and the introduction of a bulky substituent at position 6 of the purine, on the biological effects. Their inhibition against isolated HER2 was studied and the structure-activity relationships have been confirmed by molecular modelling studies. The most potent compound against isolated HER2 is 9a with an IC50 of 7.31 mu M. We have investigated the effects of the target compounds on cell proliferation. The most active compound (7c) against all the tumour cell lines studied (IC50 0.42-0.86 mu M) does not produce any modification in the expression of pro-caspase 3, but increases the caspase 1 expression, and promotes pyroptosis.
Ämnesord
- MEDICIN OCH HÄLSOVETENSKAP -- Medicinska och farmaceutiska grundvetenskaper -- Läkemedelskemi (hsv//swe)
- MEDICAL AND HEALTH SCIENCES -- Basic Medicine -- Medicinal Chemistry (hsv//eng)
- NATURVETENSKAP -- Biologi -- Biokemi och molekylärbiologi (hsv//swe)
- NATURAL SCIENCES -- Biological Sciences -- Biochemistry and Molecular Biology (hsv//eng)
Nyckelord
- Antitumour
- pyroptosis
- HER2 receptor
- molecular modelling
- benzoxazepines
Publikations- och innehållstyp
- ref (ämneskategori)
- art (ämneskategori)
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