- Zinc complex of tryptophan appended 1,4,7,10-tetraazacyclododecane as potential anticancer agent: Synthesis and evaluation
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With the rising incidences of cancer cases, the quest for new metal based anticancer drugs has led to extensive research in cancer biology. Zinc complexes of amino acid residue side chains are well recognized for hydrolysis of phosphodiester bond in DNA a
- Adhikari, Anupriya,Kumari, Neelam,Adhikari, Manish,Kumar, Nitin,Tiwari, Anjani K.,Shukla, Abha,Mishra, Anil K.,Datta, Anupama
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- Comparative evaluation of 99mTc-MBIP-X/11[C] MBMP for visualization of 18 kDa translocator protein
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An elevated translocator protein (18 kDa, TSPO) density is observed during inflammation in the brain and peripheral organs making it a viable target for imaging. Recently, our group has explored a pharmacophore skeleton acetamidobenzoxazolone for positron emission tomography (PET) and single photon emission computed tomography (SPECT) applications to target TSPO. 2-(2-(5-Bromo/chloro benzoxazolone)acetamide)-3-(1H-indol-3-yl)propionate (MBIP-Br/Cl) were synthesized by using tryptophan methyl ester and compared with 2-[5-(4-methoxyphenyl)-2-oxo-1,3-benzoxazol-3(2H)-yl]-N-methyl-N-phenyl acetamide (MBMP) through tracer techniques. Computational docking showed similar results for MBIP-Br/Cl in comparison to MBMP. Their ex vivo and in vivo biodistributions were assessed in TSPO-rich organs as well as their release kinetics 0-120 min post injection. The ex vivo biodistribution showed a 7 fold higher uptake (5.16%ID per g vs. 0.72%ID per g) in the heart and a 2.5 fold higher uptake (12.91%ID per g vs. 4.69%ID per g) in the lungs for 99mTc-MBIP-Cl compared to that of 99mTc-MBIP-Br at 15 min. These findings demonstrated that 99mTc-MBIP-Cl has improved pharmacokinetic properties compared to 99mTc-MBIP-Br for SPECT application and is comparable to [11C]MBMP.
- Srivastava, Pooja,Kumari, Neelam,Kakkar, Dipti,Kaul, Ankur,Kumar, Pravir,Tiwari, Anjani K.
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- Evaluation of methionine and tryptophan derivatised vehicles: Met-ac-TE3A / Trp-ac-TE3A for tumor imaging
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Two novel amino acid (methionine and tryptophan) appended 1,4,8,11-tetraazacyclotetradecane triacetate (TE3A) compounds Met-ac-TE3A and Trp-ac-TE3A were synthesized and evaluated for imaging applications. The pharmacokinetics of these compounds was analyzed by 99mTc labeled tracer methods. In vitro human serum stability of 99mTc labeled Met-ac-TE3A/Trp-ac-TE3A was found to be 96.5% and 96.0% after 24 h respectively. Blood kinetics of both the labeled probes on normal rabbits showed biphasic clearance. The tumor (EAT cell line) grafted in balb/c mice were readily identifiable in the gamma images. Biodistribution revealed significant tumor uptake and good contrast in the EAT tumor bearing mice and also showed high tumor/muscles ratio which is a requisite condition to work as SPECT-radiopharmaceutical for tumor imaging. To look its future applicability for therapy using M+2 and M+3 metal ions, we performed thermodynamic stability constants of complexes derived from Met-ac-TE3A and Trp-ac-TE3A with CuII and LnIII metal ions.
- Singh, Sweta,Tiwari, Anjani K.,Varshney, Raunak,Mathur, Rashi,Hazari, Puja P.,Singh,Mishra, Anil K.
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- Modified benzoxazolone (ABO-AA) based single photon emission computed tomography (SPECT) probes for 18 kDa translocator protein
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Acetamidobenzoxazolone (ABO) has been modified to ABO-AA, 2-(2-(5-bromo/chloro benzoxazolone)acetamide)-3-(1H-indol-3-yl)propionate to improve pharmacokinetics and lipophilicity (log p = 2.04). The final compound was synthesized in better yield and in few
- Srivastava, Pooja,Kakkar, Dipti,Kumar, Pravir,Tiwari, Anjani Kumar
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- Compound containing indole structure as well as preparation method and application thereof
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According to the indole structure-containing compound and the preparation method thereof, the indole structure-containing compound has high biological activity on soil-borne pathogenic bacteria, fungi and nematodes, can be widely applied to prevention and treatment of soil-borne diseases, and provides material guarantee for safe production of crops.
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Paragraph 0057-0059
(2022/01/10)
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- Diketopiperazine acylhydrazone derivatives, preparation method thereof and application of diketopiperazine acylhydrazone derivatives in prevention and treatment of plant viruses, sterilization and insect killing
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The invention relates to diketopiperazine acylhydrazone derivatives, a preparation method thereof and application of the diketopiperazine acylhydrazone derivatives in prevention and treatment of plantviruses, insect killing and sterilization. The meanings of groups in the general formula of the derivatives are shown in the description. The diketopiperazine acylhydrazone derivatives has excellentactivity of plant virus resistance, and also has broad-spectrum bactericidal activity and insecticidal activity.
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Paragraph 0056; 0057; 0060; 0061
(2020/02/17)
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- Synthesis of 3,4-Bridged Indoles by Photocyclisation Reactions. Part 1. Photocyclisation of Halogenoacetyl Tryptophan Derivatives
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Although irradiation of N-chloroacetyltryptophan results in a poor yield of photocyclisation to the indole 4-position due to competing cyclisation to C-2, the photocyclisation of (dichloroacetyl)tryptophan derivatives gives, after addition of a nucleophile in work-up, 7-substituted pyrrolobenzazocines in good yield and with trans-stereospecificity.N-(Trichloroacetyl)tryptophan derivatives also undergo photocyclisation to give 3,4-bridged indoles.The structures of the azocinoindoles 13, 21, 22 and 35, and the azepinoindole 15 were confirmed by X-ray crystallography.In one case the preparation of a cycloalkaindole was possible by the irradiation of the α-chloro amide of an indol-3-yl alkanoic acid.
- Beck, Anthony L.,Mascal, Mark,Moody, Christopher J.,Slawin, Alexandra M. Z.,Williams, David J.,Coates, William J.
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p. 797 - 812
(2007/10/02)
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