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1.
Chem Biol Drug Des ; 103(2): e14484, 2024 02.
Article in English | MEDLINE | ID: mdl-38355143

ABSTRACT

A series of alkynylated pyrrole derivatives were meticulously designed, drawing inspiration from the structure of 3-alkynylpyrrole-2,4-dicarboxylates, which were synthesized via a cyclization process involving methylene isocyanides and propiolaldehydes under mild conditions. These derivatives were subsequently subjected to evaluation for their anticancer properties against a panel of cell lines, including U251, A549, 769-P, HepG2, and HCT-116. According to the detailed analysis of structure-activity relationship, compound 12l emerged as the most promising molecule, with IC50 values of 2.29 ± 0.18 and 3.49 ± 0.30 µM toward U251 and A549 cells, respectively. Subsequent mechanistic investigations revealed that compound 12l exerts its effects by arresting the cell cycle in the G0/G1 phase and inducing apoptosis specifically in A549 cells. These innovative alkynylated pyrrole derivatives hold the potential to serve as a valuable template for the discovery of novel anticancer molecules.


Subject(s)
Antineoplastic Agents , Antineoplastic Agents/chemistry , Cell Line, Tumor , Pyrroles/chemistry , Drug Screening Assays, Antitumor , Structure-Activity Relationship , Apoptosis , Cell Proliferation , Molecular Structure , Drug Design
2.
Opt Express ; 31(8): 13455-13471, 2023 Apr 10.
Article in English | MEDLINE | ID: mdl-37157484

ABSTRACT

The practical Kramers-Kronig (KK) receiver has been a competitive receiving technique in the data-center, medium reach, and even long-haul metropolitan networks. Nevertheless, an extra digital resampling operation is required at both ends of the KK field reconstruction algorithm due to the spectrum broadening caused by adopting the nonlinear function. Generally, the digital resampling function can be implemented by using linear interpolation (LI-ITP), the Lagrange cubic interpolation (LC-ITP), the spline cubic interpolation (SC-ITP), time-domain anti-aliasing finite impulse response (FIR) filter method (TD-FRM) scheme, and fast Fourier transform (FFT)-based scheme. However, the performance and the computational complexity analysis of different resampling interpolation schemes in the KK receiver have not been thoroughly investigated yet. Different from the interpolation schemes of conventional coherent detection, the interpolation function of the KK system is followed by the nonlinear operation, which will broaden the spectrum significantly. Due to the frequency-domain transfer function of different interpolation schemes, the broadened spectrum will have a potential spectrum aliasing, which will cause serious inter-symbol interference (ISI) and further impair the KK phase retrieval performance. We experimentally investigate the performance of different interpolation schemes under different digital up-sampling rates (i.e. the computational complexity) as well as the cut-off frequency, the tap number of the anti-aliasing filter, and the shape factor of the TD-FRM scheme in a 112-Gbit/s SSB DD 16-QAM system over 1920-km Raman amplification (RFA)-based standard single-mode fiber (SSMF). The experimental results involve that the TD-FRM scheme outperforms other interpolation schemes and the complexity is reduced by at least 49.6%. In fiber transmission results, take 20% soft decision-forward error correction (SD-FEC) of 2×10-2 as the threshold, the LI-ITP and LC-ITP schemes only reach 720-km while others can reach up to 1440-km.

3.
Tumour Biol ; 36(11): 8341-8, 2015 Nov.
Article in English | MEDLINE | ID: mdl-26014519

ABSTRACT

Although the risk of neurological cancer (NC) is age-dependent, few studies have evaluated the prognostic value of age in determining NC survival in a large population. The aim of this retrospective study was to compare the long-term survival of young and elderly NC patients. We searched the Surveillance, Epidemiology, and End-Results database and identified 22,393 patients who were diagnosed with NC between 1988 and 2003 and were treated with surgery. Patients were categorized as young (≤40 years old) or elderly (>40 years old), and 5-year NC-specific survival (NCSS) data were obtained for each patient. A Kaplan-Meier survival analysis and the Cox proportional hazards model were used to analyze long-term survival outcomes and risk factors. The two groups differed significantly in terms of pathological grade, histological type, stage, and tumor size (P < 0.001). A difference in 5-year NCSS rates (63.8 and 19.0% in young and elderly patients, respectively) was detected by uni- and multivariate analyses. A stratified analysis of age on cancer survival revealed significant differences at T1-T4 stages. Age has prognostic value for determining NC risk. NCSS is higher in young than in elderly NC patients.


Subject(s)
Age Factors , Neoplasms/pathology , Nervous System Diseases/pathology , Prognosis , Adult , Aged , Aged, 80 and over , Female , Humans , Kaplan-Meier Estimate , Male , Middle Aged , Neoplasms/diagnosis , Neoplasms/epidemiology , Nervous System Diseases/diagnosis , Nervous System Diseases/epidemiology , Risk Factors
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